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HERO ID
7357291
Reference Type
Journal Article
Title
Synthesis and cytotoxicity of new thiazolo[4,5-b]pyridine-2(3H)-one derivatives based on alpha,beta-unsaturated ketones and alpha-ketoacids
Author(s)
Lozynskyi, A; Zimenkovsky, B; Radko, L; Stypula-Trebas, S; Roman, O; Gzella, AK; Lesyk, R
Year
2018
Is Peer Reviewed?
Yes
Journal
Chemical Papers / Chem Zvesti
ISSN:
0366-6352
EISSN:
1336-9075
Volume
72
Issue
3
Page Numbers
669-681
DOI
10.1007/s11696-017-0318-1
Web of Science Id
WOS:000425783100015
Abstract
A series of thiazolo[4,5-b]pyridin-2(3H)-one derivatives were obtained via [3 + 3]-cyclization of 4-amino-5H-thiazol-2-one and alpha,beta-unsaturated ketones or alpha-ketoacids. The structures of newly synthesized compounds were established by spectral data and a single-crystal X-ray diffraction analysis. Target compounds were screened for their anticancer activity according to US NCI protocols and moderate inhibitory activity against the tested cell line was confirmed. 5-Phenyl-7-(pyridin-3-yl)-3H-thiazolo[4,5-b]pyridin-2-one (3) and 2-oxo-7-thiophen-2-yl-2,3-dihydrothiazolo[4,5-b]pyridine-5-carboxylic acid (12) were screened for their cytotoxicity effects on HepG2 and Balb/c 3T3 cells which revealed promising results using MTT, NRU and TPC assays. [GRAPHICS] .
Keywords
4-Amino-5H-thiazol-2-one; Thiazolo[4,5-b]pyridin-2(3H)-one; X-ray study; Cell lines; HepG2; Balb/c 3T3
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